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更新于：2024-12-26
Icaritin
阿可拉定
更新于：2024-12-26
概要
基本信息
原研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2022-01-10), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国)、附条件批准 (中国) |
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关联
22
项与 阿可拉定 相关的临床试验NCT06644937
Single-arm Clinical Trial of TACE in Combination With Acoradine as Adjuvant Therapy After Surgery in Patients With Hepatocellular Carcinoma at High Risk of Recurrence
NCT06285149
Prospective Single-arm, Single-center Exploratory Clinical Study on Efficacy and Safety of Interventional Therapy Combined With Icaritin in First-line Treatment of Middle and Advanced HCC in Child Grade B Patients
NCT06269445
The Efficacy and Safety of Lcaritin Combined With Bevacizumab and FOLFIRI in Treatment of Liver Metastases From Colorectal Cancer: A Prospective, Single-arm Study
100 项与 阿可拉定 相关的临床结果
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100 项与 阿可拉定 相关的转化医学
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100 项与 阿可拉定 相关的专利（医药）
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333
项与 阿可拉定 相关的文献（医药）2025-04-01BIOMATERIALS
Pulmonary delivery of dual-targeted nanoparticles improves tumor accumulation and cancer cell targeting by restricting macrophage interception in orthotopic lung tumors
Article
作者: Liao, Yonghong ; Sun, Tingting ; Liao, Yong-Hong ; Ma, Siqi ; Wang, Chenao ; Wei, Jia-Xing ; Sun, Ting-Ting ; Ma, Si-Qi ; Ge, Di ; Wei, Jiaxing ; Li, Yunfei ; Chen, Xiaoyuan ; Wang, Chen-Ao ; Li, Yun-Fei
Despite the recognized potential of inhaled nanomedicines to enhance and sustain local drug concentrations for lung cancer treatment, the influence of macrophage uptake on targeted nanoparticle delivery to and within tumors remains unclear. Here, we developed three ligand-coated nanoparticles for pulmonary delivery in lung cancer therapy: phenylboronic acid-modified nanoparticles (PBA-NPs), PBA combined with folic acid (FA-PBA-NPs), and PBA with mannose (MAN-PBA-NPs). In vitro, MAN-PBA-NPs were preferentially internalized by macrophages, whereas FA-PBA-NPs exhibited superior uptake by cancer cells compared to macrophages. Following intratracheal instillation into mice with orthotopic Lewis lung carcinoma tumors, all three nanoparticles showed similar lung retention. However, MAN-PBA-NPs were more prone to interception by lung macrophages, which limited their accumulation in tumor tissues. In contrast, both PBA-NPs and FA-PBA-NPs achieved comparable high tumor accumulation (∼11.3% of the dose). Furthermore, FA-PBA-NPs were internalized by ∼30% of cancer cells, significantly more than the 10-18% seen with PBA-NPs or MAN-PBA-NPs. Additionally, FA-PBA-NPs loaded with icaritin effectively inhibited the Wnt/β-catenin pathway, resulting in superior anti-tumor efficacy through targeted cancer cell delivery. Overall, FA-PBA-NPs demonstrated advantageous competitive uptake kinetics by cancer cells compared to macrophages, enhancing tumor targeting and therapeutic outcomes.
2024-12-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Icaritin production from Epimedium folium extract by a one-pot enzymatic cascade of a multifunctional glycosidase and rhamnosidase
Article
作者: Dang, Weifan ; Zhang, Jingjing ; Zhong, Peng ; Lu, Qiwei ; Zhao, Daxin ; Wang, Cong ; Yan, Xiaohui ; Jia, Jianhua ; Huang, Jing ; Yang, Yufan ; Zhang, Chengyu
Icaritin (ICT), a compound with diverse biological activities derived from Epimedium folium, is typically present in low concentrations in EFs. However, the abundant glycosyl-modified ICT compounds facilitate its transformation into ICT. Current biocatalytic production faces challenges, including low conversion rates and limited enzyme activity. This study developed a one-pot enzymatic cascade strategy for directly biotransform crude extracts of Epimedium folium (EEF) to produce ICT. The feasibility of catalyzing different ICT-related compounds in EEF was validated through molecular docking and substrate reactions. The selected glycosidase exhibited simultaneous activities as a glucosidase, xylosidase, and α-1,6-rhamnosidase, with the rhamnosidase showing outer-rhamnosidic activity and weak glucosidase activity. By using EFs as the substrate and employing whole-cells (Escherichia coli) containing LacS and BtRha proteins for synergistic catalysis, icariin can be efficiently synthesized within 6 h, achieving a conversion rate of 100 %. The enzymatic cascade for ICT production from crude extracts was elucidated by analyzing catalytic intermediates via HPLC. Compared to strategies using single or traditional multi-enzyme applications, this method shows advantages of ease to operation, high efficiency, and large production yield performance. This method has the potential to become an eco-friendly catalytic strategy for the large-scale production of icaritin.
2024-12-01INTERNATIONAL IMMUNOPHARMACOLOGY
Synergistic effect and mechanism of monoacylglycerol lipase inhibitor and Icaritin in the treatment of ulcerative colitis
Article
作者: Liu, Yifan ; Zhang, Guimin ; Liu, Mingfei ; Li, Meng ; Li, Shirong ; Wang, Kun ; Cui, Deyu ; Shen, Mengmeng ; Lu, Xiaoyan ; Tang, Hongguang ; Yao, Jingchun
Ulcerative colitis (UC) is a chronic, relapsing nonspecific intestinal inflammatory disease. It is difficult for a single drug to treat UC effectively and maintain long-term efficacy. There is an urgent need to find new drugs and treatment strategies. MAGL11 is a new kind of single acylglycerol lipase (MAGL) inhibitor. Icaritin (Y003) is the major metabolite of icariin in vivo. Several studies have confirmed the role of MAGL inhibitors and icariin in anti-inflammatory and regulation of intestinal stability. Therefore, this study adopted a new strategy of combining MAGL inhibitor with Icaritin to further explore the role and mechanism of drugs in the treatment of UC. Enzyme-linked immunosorbent assay (ELISA), hematoxylin-eosin staining (HE), immunohistochemical (IHC) and Western blot were used to detect the synergistic protective effects of MAGL11 and Y003 on intestinal pathological injury, intestinal mucosal permeability and inflammation in UC mice. 16S rDNA sequencing was used to detect the synergistic effect of MAGL11 and Y003 on gut microbiota. The effects of MAGL11 and Y003 combined therapy on serum and fecal metabolism of UC mice were analyzed by untargeted metabolomics. Proteomics method was applied to investigate the molecular mechanisms underlying MAGL11 and Y003 synergy in the treatment of UC. The results showed that MAGL11 and Y003 could synergistically improve the clinical symptoms, reduce intestinal inflammation and pathological damage, and improve intestinal mucosal permeability in UC mice. The mechanism study found that MAGL11 and Y003 could synergistically inhibit Toll-like receptors 4 (TLR4) / Myeloid differentiation primary response gene (Myd88)/Nuclear factor kappa-B (NF-κB) pathway and further regulate gut microbiota imbalance and metabolic disorders to treat UC.
100 项与 阿可拉定 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 肝细胞癌 | 中国 | 2022-01-10 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 不可切除的肝细胞癌 | 临床3期 | 中国 | 2022-12-12 | |
| 肝癌 | 临床3期 | 中国 | 2022-01-30 | |
| 晚期肝细胞癌 | 临床3期 | 中国 | 2017-09-08 | |
| 乙型肝炎病毒相关肝细胞癌 | 临床3期 | 中国 | 2017-09-08 | |
| 晚期癌症 | 临床1期 | 中国 | 2011-11-28 | |
| 晚期恶性实体瘤 | 临床1期 | 中国 | 2011-11-01 | |
| 晚期乳腺癌 | 临床1期 | 中国 | 2010-11-01 | |
| 转移性乳腺癌 | 临床1期 | 中国 | 2010-11-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 283 | 簾範網襯窪鹹鹹遞窪範(築願廠襯製願網觸蓋淵) = 觸艱網觸顧廠鏇膚餘顧 膚觸繭範觸鹹衊鏇製構 (選艱醖糧遞簾簾積鹹製 ) 更多 | 积极 | 2021-05-20 | |||
huachashu | 簾範網襯窪鹹鹹遞窪範(築願廠襯製願網觸蓋淵) = 選鹽鑰鹽鏇鹹鬱醖鏇鹹 膚觸繭範觸鹹衊鏇製構 (選艱醖糧遞簾簾積鹹製 ) 更多 | ||||||
临床1期 | 20 | 繭餘鹽蓋鹹夢遞顧鏇網(鬱繭壓艱窪襯簾夢壓鏇) = 願鏇醖艱鹹繭衊鏇繭壓 鹽顧餘憲遞構膚簾夢鑰 (簾窪窪範顧餘餘構艱構 ) 更多 | 积极 | 2019-03-28 | |||
N/A | - | - | 範築簾範衊獵鬱膚遞淵(膚餘夢繭廠範繭繭醖壓) = 顧鬱艱憲窪齋鬱醖獵膚 憲齋窪壓獵顧網淵餘繭 (壓蓋鬱糧繭壓網網艱鬱 ) 更多 | 积极 | 2015-04-17 |
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